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Keywords:

  • arenes;
  • copper;
  • homogeneous catalysis;
  • ketones;
  • synthetic methods
Thumbnail image of graphical abstract

No activation needed: The first efficient method for direct α-arylation of non-activated or non-protected family of enolizable ketones with simple aryl iodides employs a catalytic copper system. The method shows potential for the easy and step-economical synthesis of tamoxifen, the most commonly administrated drug for the management of breast cancer. R, R′, R′′ = electron-donating or electron-withdrawing groups.